JP7260723B2 - ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン - Google Patents

ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン Download PDF

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JP7260723B2
JP7260723B2 JP2022563041A JP2022563041A JP7260723B2 JP 7260723 B2 JP7260723 B2 JP 7260723B2 JP 2022563041 A JP2022563041 A JP 2022563041A JP 2022563041 A JP2022563041 A JP 2022563041A JP 7260723 B2 JP7260723 B2 JP 7260723B2
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compound
cancer
her2
pharmaceutically acceptable
salt
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JP2023512343A (ja
Inventor
ヴィルディング，ビルギット
ブーセ，ディートリヒ
エンゲルハルト，ハーラルト
フックス，ユリアン
ノイミュラー，ラルフ
ペトロンスキ，マルク
シャルン，ディルク
トロイ，マティアス
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ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2022563041A 2020-04-24 2021-04-07 ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン Active JP7260723B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2023062141A JP2023085489A (ja) 2020-04-24 2023-04-06 ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20171221 2020-04-24
EP20171221.3 2020-04-24
PCT/EP2021/059015 WO2021213800A1 (en) 2020-04-24 2021-04-07 [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS

Related Child Applications (1)

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JP2023062141A Division JP2023085489A (ja) 2020-04-24 2023-04-06 ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン

Publications (2)

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JP2023512343A JP2023512343A (ja) 2023-03-24
JP7260723B2 true JP7260723B2 (ja) 2023-04-18

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JP2022563041A Active JP7260723B2 (ja) 2020-04-24 2021-04-07 ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン
JP2023062141A Pending JP2023085489A (ja) 2020-04-24 2023-04-06 ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン

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US (3) US11608343B2 (enExample)
EP (2) EP4566611A3 (enExample)
JP (2) JP7260723B2 (enExample)
KR (2) KR20250016507A (enExample)
CN (13) CN118388487A (enExample)
AR (1) AR121779A1 (enExample)
AU (1) AU2021260721A1 (enExample)
BR (1) BR112022021514A2 (enExample)
CA (1) CA3173602A1 (enExample)
CL (1) CL2022002579A1 (enExample)
CO (1) CO2022015054A2 (enExample)
CR (1) CR20220537A (enExample)
DK (1) DK4139309T5 (enExample)
DO (1) DOP2022000189A (enExample)
EC (1) ECSP22072777A (enExample)
ES (1) ES3013860T3 (enExample)
FI (1) FI4139309T3 (enExample)
HR (1) HRP20250426T1 (enExample)
HU (1) HUE070805T2 (enExample)
IL (2) IL297490B2 (enExample)
LT (1) LT4139309T (enExample)
MA (1) MA59373B1 (enExample)
MX (1) MX2022013223A (enExample)
PE (1) PE20230827A1 (enExample)
PH (1) PH12022552745A1 (enExample)
PL (1) PL4139309T3 (enExample)
PT (1) PT4139309T (enExample)
RS (1) RS66557B1 (enExample)
SI (1) SI4139309T1 (enExample)
SM (1) SMT202500164T1 (enExample)
TW (1) TW202206432A (enExample)
WO (1) WO2021213800A1 (enExample)

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JP7626773B2 (ja) * 2020-02-03 2025-02-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン
US11608343B2 (en) 2020-04-24 2023-03-21 Boehringer Ingelheim International Gmbh Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors
TW202214641A (zh) 2020-06-30 2022-04-16 美商艾瑞生藥股份有限公司 Ｈｅｒ２突變抑制劑
BR112023021111A2 (pt) 2021-04-13 2023-12-19 Nuvalent Inc Composto, composição farmacêutica, método de tratamento de câncer, método para inibir seletivamente her2, método de regulação de um nível de her2, método para aumentar um nível de her2, método de diminuição da fosforilação de her2
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WO2023154124A1 (en) * 2022-02-09 2023-08-17 Enliven Therapeutics, Inc. Acylated heterocyclic quinazoline derivatives as inhibitors of erbb2
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WO2024133289A1 (en) 2022-12-22 2024-06-27 Boehringer Ingelheim International Gmbh Solid dispersion of a her2 inhibitor
CN120456906A (zh) 2022-12-22 2025-08-08 勃林格殷格翰国际有限公司 Her2抑制剂的固体分散体的给药安排方案
WO2024200637A2 (en) 2023-03-29 2024-10-03 Boehringer Ingelheim International Gmbh Dosing schedule of a her2 inhibitor
TW202504611A (zh) 2023-03-30 2025-02-01 美商銳新醫藥公司 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
TW202510886A (zh) 2023-05-31 2025-03-16 德商百靈佳殷格翰國際股份有限公司 作為用於預測癌症治療反應性之生物標記之存活素
CN116903615A (zh) * 2023-06-21 2023-10-20 江苏丽源医药有限公司 一种妥卡替尼及其中间体的制备方法
TW202521538A (zh) 2023-07-28 2025-06-01 德商百靈佳殷格翰國際股份有限公司 製備her2抑制劑之方法
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
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MX2022013223A (es) 2022-11-14
CN118388495A (zh) 2024-07-26
CN118388492A (zh) 2024-07-26
IL297490A (en) 2022-12-01
LT4139309T (lt) 2025-02-25
SMT202500164T1 (it) 2025-05-12
EP4566611A2 (en) 2025-06-11
DK4139309T3 (da) 2025-04-28
PL4139309T3 (pl) 2025-05-05
CR20220537A (es) 2022-12-06
ECSP22072777A (es) 2022-10-31
JP2023085489A (ja) 2023-06-20
CN118619956A (zh) 2024-09-10
JP2023512343A (ja) 2023-03-24
FI4139309T3 (fi) 2025-03-04
AU2021260721A1 (en) 2022-09-15
MA59373B1 (fr) 2025-02-28
CN118388488A (zh) 2024-07-26
CA3173602A1 (en) 2021-10-28
DK4139309T5 (da) 2025-10-27
US20210332054A1 (en) 2021-10-28
ES3013860T9 (en) 2025-10-28
IL297490B2 (en) 2025-10-01
EP4139309B9 (en) 2025-09-10
CN118388489A (zh) 2024-07-26
RS66557B1 (sr) 2025-03-31
PE20230827A1 (es) 2023-05-19
CN118388491A (zh) 2024-07-26
US20230374021A1 (en) 2023-11-23
CN118388494A (zh) 2024-07-26
CN118307543A (zh) 2024-07-09
EP4566611A3 (en) 2025-09-10
ES3013860T3 (en) 2025-04-15
US11608343B2 (en) 2023-03-21
CN118388490A (zh) 2024-07-26
EP4139309B1 (en) 2025-01-29
KR20250016507A (ko) 2025-02-03
HRP20250426T1 (hr) 2025-06-06
KR102759974B1 (ko) 2025-01-24
CN118388493A (zh) 2024-07-26
KR20230005263A (ko) 2023-01-09
CO2022015054A2 (es) 2023-02-16
BR112022021514A2 (pt) 2023-01-24
CN118388487A (zh) 2024-07-26
SI4139309T1 (sl) 2025-03-31
CN115485277B (zh) 2024-05-14
WO2021213800A1 (en) 2021-10-28
CN118307544A (zh) 2024-07-09
IL320477A (en) 2025-06-01
DOP2022000189A (es) 2022-09-30
PH12022552745A1 (en) 2024-03-25
PT4139309T (pt) 2025-02-17
US20250122204A1 (en) 2025-04-17
HUE070805T2 (hu) 2025-07-28
TW202206432A (zh) 2022-02-16
CL2022002579A1 (es) 2023-05-19
EP4139309A1 (en) 2023-03-01
AR121779A1 (es) 2022-07-06
CN115485277A (zh) 2022-12-16
IL297490B1 (en) 2025-06-01

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